Synthetic schemes for the naturally occurring antibiotic, naphthyridinomycin, and the antitumor agent, saframycin B, are proposed. Both compounds possess characteristic quinone and piperazine structures in common. In order to develop a general synthetic route to this type of compound, a novel synthetic method for cis disubstituted 2,5-piperazinediones is proposed. Using the proposed methods, it is possible to synthesize a variety of quinone amine compounds which might exhibit higher antibiotic and/or antitumor activity than their parent compounds.